diazepam [Ligand Id: 3364] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL12 (NSC-77518, Scriptopam, Atensine, Diazepam Intensol, Dizac, Paxel, Q-Pam, Apozepam, Vivol, Alupram 10, Tranimul, Solis, Relanium, Dialar Fte, Diastat, Diazepam, NSC-169897, E-Pam, Dialar, Alupram 5, Stesolid, Alupram 2, Valium, Serenack, Valclair, WY-3467, Tensium, Ro-52807, Valrelease, Diastat Acudial, RO-5-2807, LA-III, Diazepam civ)
  • Acetylcholinesterase in Electrophorus electricus [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
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  • Aldo-keto reductase family 1 member C1 in Human [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
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  • Aldo-keto reductase family 1 member C2 in Human [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
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  • AKR1C3/Aldo-keto-reductase family 1 member C3 in Human [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
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  • CCK1 receptor/Cholecystokinin A receptor in Rat [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
  • Cholecystokinin A receptor in Guinea pig [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
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  • fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
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  • GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human [ChEMBL: CHEMBL2111392] [GtoPdb: 404410414] [UniProtKB: P14867P18505P18507]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2095167] [GtoPdb: 414404411] [UniProtKB: P18508P62813P63138]
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  • GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094121] [GtoPdb: 404414412] [UniProtKB: P14867P18507P28472]
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  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit in Human [GtoPdb: 414405411] [UniProtKB: P18507P47869P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111327] [GtoPdb: 414405411] [UniProtKB: P18508P23576P63138]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094130] [GtoPdb: 414412405] [UniProtKB: P18507P28472P47869]
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  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111339] [GtoPdb: 414406411] [UniProtKB: P18507P34903P47870]
  • GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111343] [GtoPdb: 414406411] [UniProtKB: P18508P20236P63138]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094120] [GtoPdb: 414412406] [UniProtKB: P18507P28472P34903]
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  • GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β3 subunit/GABA A receptor alpha-5/beta-3/gamma-2 in Rat [ChEMBL: CHEMBL2111374] [GtoPdb: 414408412] [UniProtKB: P18508P19969P63079]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α5 subunit/GABA-A receptor; alpha-5/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2094122] [GtoPdb: 414412408] [UniProtKB: P18507P28472P31644]
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  • GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABAA receptor α6 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Human [ChEMBL: CHEMBL2111370] [GtoPdb: 414411409] [UniProtKB: P18507P47870Q16445]
  • GABAA receptor γ2 subunit/GABAA receptor α6 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-6/beta-2/gamma-2 in Rat [ChEMBL: CHEMBL2111365] [GtoPdb: 414409411] [UniProtKB: P18508P30191P63138]
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  • GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α6 subunit/GABA-A receptor; alpha-6/beta-3/gamma-2 in Human [ChEMBL: CHEMBL2095190] [GtoPdb: 414412409] [UniProtKB: P18507P28472Q16445]
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  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Human [ChEMBL: CHEMBL1962] [GtoPdb: 404] [UniProtKB: P14867]
  • GABAA receptor α1 subunit/GABA receptor alpha-1 subunit in Rat [ChEMBL: CHEMBL343] [GtoPdb: 404] [UniProtKB: P62813]
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  • GABAA receptor α2 subunit in Human [GtoPdb: 405] [UniProtKB: P47869]
  • GABAA receptor α2 subunit/GABA receptor alpha-2 subunit in Rat [ChEMBL: CHEMBL341] [GtoPdb: 405] [UniProtKB: P23576]
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  • GABAA receptor α3 subunit in Human [GtoPdb: 406] [UniProtKB: P34903]
  • GABAA receptor α3 subunit/GABA receptor alpha-3 subunit in Rat [ChEMBL: CHEMBL328] [GtoPdb: 406] [UniProtKB: P20236]
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  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Human [ChEMBL: CHEMBL5112] [GtoPdb: 408] [UniProtKB: P31644]
  • GABAA receptor α5 subunit/GABA receptor alpha-5 subunit in Rat [ChEMBL: CHEMBL300] [GtoPdb: 408] [UniProtKB: P19969]
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  • GABAA receptor γ1 subunit/GABA receptor gamma-1 subunit in Rat [ChEMBL: CHEMBL296] [GtoPdb: 413] [UniProtKB: P23574]
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  • Translocator protein/Peripheral-type benzodiazepine receptor in Rat [ChEMBL: CHEMBL4552] [GtoPdb: 2879] [UniProtKB: P16257]
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  • TRH1 receptor in Rat [GtoPdb: 363] [UniProtKB: Q01717]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275]
ChEMBL Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) assessed as inhibition of ATCh hydrolysis by Ellman method B 4.89 pKi 13000 nM Ki Med Chem Res (2005) 14: 297-308
Aldo-keto reductase family 1 member C1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5905] [UniProtKB: Q04828]
ChEMBL Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). B 5.25 pIC50 5600 nM IC50 US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016)
Aldo-keto reductase family 1 member C2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5847] [UniProtKB: P52895]
ChEMBL Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). B 5.62 pIC50 2400 nM IC50 US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016)
AKR1C3/Aldo-keto-reductase family 1 member C3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4681] [GtoPdb: 1382] [UniProtKB: P42330]
ChEMBL Discontinuous Radiometric Assay: Compounds may be evaluated as selective reversible inhibitors of AKR1C3 by screening them against homogeneous recombinant AKR1C1-AKR1C4 expressed in E. coli. In each case, a discontinuous radiometric assay may be used to monitor the inhibition of progesterone reduction (20-ketosteroid reduction) catalyzed by AKR1C1, the inhibition of Δ4-AD reduction (17-ketosteroid reduction) catalyzed by AKR1C3, and the inhibition of 5α-DHT reduction (3-ketosteroid reduction) catalyzed by AKR1C2 and AKR1C4 (by measuring the formation of 20α-hydroxyprogesterone, testosterone or 3α-androstanediol by radiochromatography). Secondary screens of the compounds of interest include: (a) a full-screen against all nine human recombinant AKR enzymes to ensure there are no-intended off-target effects (in this context AKR1B10 (retinal reductase; SEQ ID NO:5) has been shown to be potently inhibited by N-phenylanthranilates) (Endo et al., 2010, Biol. Pharm. Bull. 33:886-90); (b) a screen against COX-1 and COX-2 to reaffirm that compounds do not act as NSAIDs; and (c) an expanded screen against other nuclear receptors (especially other steroid hormone receptors). B 4.08 pIC50 84000 nM IC50 US-9271961-B2. Bifunctional AKR1C3 inhibitors/androgen receptor modulators and methods of use thereof (2016)
CCK1 receptor/Cholecystokinin A receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2871] [GtoPdb: 76] [UniProtKB: P30551]
ChEMBL Half-maximal inhibition of [125I]CCK-33 binding to cholecystokinin A receptor from rat pancreatic tissue B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1988) 31: 2235-2246 [PMID:2848124]
Cholecystokinin A receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3501] [UniProtKB: Q63931]
ChEMBL Half-maximal inhibition of [125I]CCK-33 binding to guinea pig brain(cortex) cholecystokinin receptor B 4 pIC50 >100000 nM IC50 J. Med. Chem. (1987) 30: 1229-1239 [PMID:2885419]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 5.3 pKi 5011.87 nM Ki Med Chem Res (2005) 14: 297-308
ChEMBL Inhibition of Equus caballus (horse) serum butyrylcholinesterase (BChE) assessed as inhibition of BTCh hydrolysis by Ellman method B 7.37 pKi 43 nM Ki Med Chem Res (2005) 14: 297-308
fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692]
ChEMBL Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP high binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay B 6.27 pKi 531 nM Ki J. Med. Chem. (2008) 51: 3755-3764 [PMID:18533710]
GABAA receptor α1 subunit/GABAA receptor β1 subunit/GABAA receptor γ2 subunit/GABA A receptor alpha-1/beta-1/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111392] [GtoPdb: 404410414] [UniProtKB: P14867P18505P18507]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Displacement of [3H]Flumazenil from human GABA-Aalpha1 receptor plus beta-2-gamma-2 expressed in HEK293 cells B 7.92 pKi 12 nM Ki J. Med. Chem. (2006) 49: 2526-2533 [PMID:16610795]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095172] [GtoPdb: 404414411] [UniProtKB: P14867P18507P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Displacement of [3H]Flunitrazepam from GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in Sf9 cells B 7.89 pKi 13 nM Ki J. Med. Chem. (1996) 39: 158-175 [PMID:8568803]
ChEMBL Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-1-beta-2-gamma-2 expressed in L(tk-)cells B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Binding affinity to human alpha1beta2gamma2 GABA receptor expressed in Xenopus laevis oocytes B 7.07 pEC50 85 nM EC50 Bioorg. Med. Chem. (2010) 18: 8374-8382 [PMID:20980155]
GABAA receptor γ2 subunit/GABAA receptor α1 subunit/GABAA receptor β2 subunit/GABA-A receptor; alpha-1/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095167] [GtoPdb: 414404411] [UniProtKB: P18508P62813P63138]
ChEMBL Binding affinity for mutant rat GABA-A receptor alpha-1-(arg)-beta-2-gamma-2 subunits expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.8 pKi 16 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.85 pKi 14 nM Ki J. Med. Chem. (2002) 45: 5710-5720 [PMID:12477354]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.85 pKi 14 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
ChEMBL Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.92 pKi 12 nM Ki Bioorg. Med. Chem. (2007) 15: 2573-2586 [PMID:17306981]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-1-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.96 pKi 11 nM Ki J. Med. Chem. (2009) 52: 3723-3734 [PMID:19469479]
ChEMBL Displacement of [3H]Ro-151788 from rat recombinant GABA alpha-5-beta-2-gamma-2 receptor expressed in HEK293 cells B 8.01 pKi 9.8 nM Ki Bioorg. Med. Chem. (2007) 15: 2573-2586 [PMID:17306981]
GABAA receptor α1 subunit/GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABA-A receptor; alpha-1/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094121] [GtoPdb: 404414412] [UniProtKB: P14867P18507P28472]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α1β1γ2. - 7.79 pKi 16.3 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Binding affinity towards human alpha-1-beta-3-gamma-2 GABA-A receptor using [3H]Ro-151788 expressed in L(tk-) cells B 7.84 pKi 14.3 nM Ki J. Med. Chem. (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity for human GABA-A receptor alpha-4-beta-3-gamma-2 subunits in L(tk-) cells B 7.85 pKi 14 nM Ki J. Med. Chem. (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-1-beta-3-gamma-2 receptor expressed in L(tk-) cells B 7.85 pKi 14 nM Ki J. Med. Chem. (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-1-beta-3-gamma-2 B 7.85 pKi 14 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-1-beta-3-gamma-2 subtype expressed in L (tk-) cells B 7.89 pKi 13 nM Ki J. Med. Chem. (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha1 in combination with beta-3-gamma-2 expressed in L(tk-) cells B 7.89 pKi 13 nM Ki J. Med. Chem. (2006) 49: 35-38 [PMID:16392789]
ChEMBL Displacement of [3H]Ro 15-1788 from recombinant human GABAA alpha-1 receptor plus beta3gamma2 expressed in L(tk-) cells B 7.89 pKi 13 nM Ki J. Med. Chem. (2006) 49: 1235-1238 [PMID:16480260]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit in Human [GtoPdb: 414405411] [UniProtKB: P18507P47869P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 7.77 pKi 16.9 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
GABAA receptor γ2 subunit/GABAA receptor α2 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-2/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111327] [GtoPdb: 414405411] [UniProtKB: P18508P23576P63138]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-2-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.7 pKi 20 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α2 subunit/GABA-A receptor; alpha-2/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094130] [GtoPdb: 414412405] [UniProtKB: P18507P28472P47869]
ChEMBL Displacement of [3H] Ro15-1788 from recombinant human GABAA alpha2 receptor plus beta-3-gamma-2 expressed in L(tk-) cells B 7.48 pKi 33 nM Ki J. Med. Chem. (2006) 49: 1235-1238 [PMID:16480260]
ChEMBL Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-2-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells B 7.58 pKi 26.2 nM Ki J. Med. Chem. (2004) 47: 3642-3657 [PMID:15214791]
ChEMBL Binding affinity for human GABA-A receptor alpha-2-beta-3-gamma-2 subunits in L(tk-) cells B 7.7 pKi 20 nM Ki J. Med. Chem. (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-2-beta-3-gamma-2 receptor expressed in L(tk-) cells B 7.7 pKi 20 nM Ki J. Med. Chem. (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity to human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-2-beta-3-gamma-2 B 7.7 pKi 20 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α2β1γ2. - 7.77 pKi 16.9 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 subtype expressed in L (tk-) cells B 8.18 pKi 6.6 nM Ki J. Med. Chem. (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Binding affinity evaluated by ability to displace [3H]-Ro-15-1788 from recombinant human Gamma-aminobutyric acid A receptor alpha-2-beta-3-gamma-2 expressed in L(tk-)cells B 8.18 pKi 6.6 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Displacement of [3H]-Ro15-1788 from human recombinant GABAA alpha2 in combination with beta3gamma2 expressed in L(tk-) cells B 8.18 pKi 6.6 nM Ki J. Med. Chem. (2006) 49: 35-38 [PMID:16392789]
ChEMBL Binding affinity to human alpha2beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes B 7.46 pEC50 35 nM EC50 Bioorg. Med. Chem. (2010) 18: 8374-8382 [PMID:20980155]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111339] [GtoPdb: 414406411] [UniProtKB: P18507P34903P47870]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.77 pKi 17 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Displacement of [3H]Flumazenil from human GABA-Aalpha3 receptor plus beta-2-gamma-2 expressed in HEK293 cells B 7.85 pKi 14 nM Ki J. Med. Chem. (2006) 49: 2526-2533 [PMID:16610795]
ChEMBL Displacement of [3H]flunitrazepam from GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in Sf9 cells B 8 pKi 10 nM Ki J. Med. Chem. (1996) 39: 158-175 [PMID:8568803]
GABAA receptor γ2 subunit/GABAA receptor α3 subunit/GABAA receptor β2 subunit/GABA A receptor alpha-3/beta-2/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111343] [GtoPdb: 414406411] [UniProtKB: P18508P20236P63138]
ChEMBL Binding affinity for rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.77 pKi 17 nM Ki J. Med. Chem. (1994) 37: 4576-4580 [PMID:7799410]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.82 pKi 15 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
ChEMBL Displacement of [3H]Ro15-1788 from rat recombinant GABA alpha-3-beta-2-gamma-2 receptor expressed in HEK293 cells B 7.85 pKi 14 nM Ki Bioorg. Med. Chem. (2007) 15: 2573-2586 [PMID:17306981]
ChEMBL Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells B 7.86 pKi 13.9 nM Ki J. Med. Chem. (2002) 45: 5710-5720 [PMID:12477354]
GABAA receptor γ2 subunit/GABAA receptor β3 subunit/GABAA receptor α3 subunit/GABA-A receptor; alpha-3/beta-3/gamma-2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094120] [GtoPdb: 414412406] [UniProtKB: P18507P28472P34903]
ChEMBL Binding affinity evaluated by ability to displace [3H]Ro-151788 from recombinant human Gamma-aminobutyric acid A receptor alpha-3-beta-3-gamma-2 expressed in L(tk-)cells B 7.48 pKi 33 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 1381-1384 [PMID:10890169]
ChEMBL Displacement of [3H]Ro-151788 from human recombinant GABAA alpha3 in combination with beta3gamma2 expressed in L(tk-) cells B 7.48 pKi 33 nM Ki J. Med. Chem. (2006) 49: 35-38 [PMID:16392789]
ChEMBL Inhibition of [3H]Ro-151788 binding to recombinant human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 subtype expressed in L (tk-) cells B 7.48 pKi 33 nM Ki J. Med. Chem. (2005) 48: 1367-1383 [PMID:15743180]
ChEMBL Binding affinity towards human gamma-aminobutyric-acid A receptor alpha-3-beta-3-gamma-2 using [3H]Ro-151788 expressed in L(tk-) cells B 7.63 pKi 23.7 nM Ki J. Med. Chem. (2004) 47: 3642-3657 [PMID:15214791]
GtoPdb Assay using recombinant GABAA channels with subunit composition; α3β1γ2. - 7.77 pKi 17 nM Ki Science (1989) 245: 1389-92 [PMID:2551039]
ChEMBL Binding affinity for human GABA-A receptor alpha-3-beta-3-gamma-2 subunits in L(tk-) cells B 7.82 pKi 15 nM Ki J. Med. Chem. (2004) 47: 1807-1822 [PMID:15027873]
ChEMBL Binding affinity for human recombinant gamma-aminobutyric-acid (GABA) A receptor alpha-3-beta-3-gamma-2 B 7.82 pKi 15 nM Ki J. Med. Chem. (2000) 43: 71-95 [PMID:10633039]
ChEMBL Displacement of [3H]Ro 15-1788 from human recombinant GABAA alpha-3-beta-3-gamma-2 receptor expressed in L(tk-) cells B 7.82 pKi 15 nM Ki J. Med. Chem. (2005) 48: 7089-7092 [PMID:16279764]
ChEMBL Binding affinity to human alpha3beta3gamma2 GABA receptor expressed in Xenopus laevis oocytes B 6.88 pEC50 131 nM EC50 Bioorg. Med. Chem. (2010) 18: 8374-8382 [PMID:20980155]
GABAA receptor γ2 subunit/GABAA receptor α5 subunit/GABAA receptor β3 subunit/GABA A receptor alpha-5/beta-3/gamma-2 in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111374] [GtoPdb: 414408412] [UniProtKB: P18508P19969P63079]
ChEMBL Binding affinity for recombinant rat GABA-A receptor alpha-5-beta-3-gamma-2 subunits expressed in HEK 293 cells B 7.96 pKi 11 nM Ki J. Med. Chem. (2003) 46: 310-313 [PMID:12519068]
ChEMBL Displacement of [3H]flumazenil from rat GABA-A alpha-5-beta-3-gamma-2 receptor expressed in HEK293 cells B 8.01